Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
نویسندگان
چکیده
Theory, Practice, and Opportunities for Central Nervous System Drug Discovery Bruce J. Melancon,†,‡,§ Corey R. Hopkins,†,∥,‡,§ Michael R. Wood,†,∥,‡,§ Kyle A. Emmitte,†,∥,‡,§ Colleen M. Niswender,†,‡,§ Arthur Christopoulos, P. Jeffrey Conn,†,‡,§ and Craig W. Lindsley*,†,∥,‡,§ †Department of Pharmacology, ‡Vanderbilt Center for Neuroscience Drug Discovery, and Vanderbilt Specialized Chemistry Center (MLPCN), Vanderbilt University Medical Center, Nashville, Tennessee 37232, United States Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Melbourne, Australia
منابع مشابه
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric systems, affinity and efficacy can be thought of in terms of energy flow between a modulator, conduit (the receptor protein), and a number of guests. These guests can be other molecules, receptors, membrane-bound pr...
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عنوان ژورنال:
- Journal of medicinal chemistry
دوره 55 4 شماره
صفحات -
تاریخ انتشار 2012